Chemical Property of CCT 244747
Chemical Property:
- PSA:114.01000
- LogP:2.29788
- Solubility.:Soluble in DMSO
- Purity/Quality:
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99%, *data from raw suppliers
CCT244747 >98% *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
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Description
CCT244747 is a potent inhibitor of checkpoint kinase 1 (Chk1; IC50 = 8 nM). It is selective for Chk1 over FLT3, Chk2, and CDK1 (IC50s = 600, >10,000, and >10,000 nM, respectively) as well as a panel of 121 additional kinases at a concentration of 10 μM. CCT244747 reverses cell cycle arrest at the G2/M phase induced by etoposide and SN-38 in HT-29 cells and gemcitabine (Item Nos. 11690 | 9003096) in SW620 cells, indicating cellular G2 checkpoint abrogation. It potentiates the genotoxicity of SN-38, gemcitabine, and etoposide in HT-29, SW620, MiaPaCa-2, and Calu-6 cells with potentiation index (PI) values ranging from 1.9-8.5, 2.6-12.2, 5-16, and 1.4-5.6, respectively. In vivo, CCT244747 (75 mg/kg), in combination with irinotecan or gemcitabine, increases the delay of tumor growth in SW620 and Calu-6 mouse xenograft models, respectively.